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| ID | Type | Description | Link |
|---|---|---|---|
| MK-1084-008 | Other Identifier | MSD | |
| CA43207 | Other Identifier | Celerion |
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The goal of this study is to learn what happens to calderasib in a healthy person's body over time, called a pharmacokinetic (PK) study. Researchers want to compare the amount of calderasib when it is taken as a single dose; with multiple doses of itraconazole, or with multiple doses of phenytoin.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: Calderasib + Itraconazole | Experimental | Part 1: In Period 1 participants receive a single dose of calderasib on Day 1 under fasting conditions. In Period 2 participants receive itraconazole once daily (QD) for 7 consecutive days (Day 1 - Day 7), plus a single dose of calderasib administered approximately 2 hours after itraconazole dosing on Day 5. There will be a washout of at least 7 days between dosing in Period 1 and the first dose in Period 2. |
|
| Part 2: Calderasib + Phenytoin | Experimental | Part 2: In Period 1 participants receive a single dose of calderasib on Day 1 under fasting conditions. In Period 2 participants receive phenytoin three times daily (TID) for 14 consecutive days (Day 1 - Day 14), plus a single dose of calderasib co-administered on the morning of Day 13. There will be a washout of at least 7 days between dosing in Period 1 and the first dose in Period 2. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Calderasib | Drug | Oral Tablet |
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| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-Time Curve from Time 0 to Infinity After Single Dosing (AUC0-Inf) of Calderasib | Blood samples will be collected to determine the AUC0-Inf of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-Time Curve from Time 0 to Last Quantifiable Sample (AUC0-last) of Calderasib | Blood samples will be collected to determine the AUC0-last of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Area Under the Concentration-Time Curve from Time 0 to 24 hours (AUC0-24) of Calderasib |
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Inclusion Criteria:
The main inclusion criteria include but are not limited to the following:
- Has body mass index (BMI) ≥18 kg/m^2 and ≤32 kg/m^2
Exclusion Criteria:
The main exclusion criteria include but are not limited to the following:
Part 1 Only:
- History or presence of ventricular dysfunction or risk factors for Torsades de Pointes (e.g., heart failure, cardiomyopathy, family history of Long QT Syndrome)
Pat 2 Only:
- History of seizure (excluding simple febrile seizure), epilepsy, severe head injury, multiple sclerosis, or other known neurological conditions
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director | Merck Sharp & Dohme LLC | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Celerion (Site 0001) | Lincoln | Nebraska | 68502 | United States |
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| Label | URL |
|---|---|
| Merck Clinical Trials Information | View source |
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| ID | Term |
|---|---|
| D017964 | Itraconazole |
| D010672 | Phenytoin |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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| Itraconazole | Drug | Oral solution |
|
| Phenytoin | Drug | Oral capsule (extended) |
|
Blood samples will be collected to determine the AUC0-24 of calderasib. |
| Pre-dose and at designated time points up to 24 hours post dose |
| Maximum Plasma Concentration (Cmax) of Calderasib | Blood samples will be collected to determine the Cmax of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Plasma Concentration at 24 Hours (C24) of Calderasib | Blood samples will be collected to determine the C24 of calderasib. | Pre-dose and at designated time points up to 24 hours post dose |
| Time to Maximum Plasma Concentration (Tmax) of Calderasib | Blood samples will be collected to determine the Tmax of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Apparent Terminal Half-life (t1/2) of Calderasib | Blood samples will be collected to determine the t1/2 of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Apparent Clearance (CL/F) of Calderasib | Blood samples will be collected to determine the CL/F of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Apparent volume of distribution during terminal phase (Vz/F) of Calderasib | Blood samples will be collected to determine the Vz/F of calderasib. | Pre-dose and at designated time points up to 72 hours post dose |
| Number of Participants Who Experience an Adverse Event (AE) | An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. The number of participants who experience an AE will be reported. | Up to approximately 41 days |
| Number of Participants Who Discontinue Study Treatment Due to an AE | An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. The number of participants who discontinue study treatment due to an AE will be reported. | Up to approximately 25 days |
| D010879 |
| Piperazines |
| D006827 | Hydantoins |
| D048289 | Imidazolidines |
| D007093 | Imidazoles |